EP3544975A4 - Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use - Google Patents
Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use Download PDFInfo
- Publication number
- EP3544975A4 EP3544975A4 EP17873155.0A EP17873155A EP3544975A4 EP 3544975 A4 EP3544975 A4 EP 3544975A4 EP 17873155 A EP17873155 A EP 17873155A EP 3544975 A4 EP3544975 A4 EP 3544975A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- btk
- bruton
- conjugation
- degradation
- methods
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 title 1
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 title 1
- 229940124291 BTK inhibitor Drugs 0.000 title 1
- 102000003960 Ligases Human genes 0.000 title 1
- 108090000364 Ligases Proteins 0.000 title 1
- 230000015556 catabolic process Effects 0.000 title 1
- 230000021615 conjugation Effects 0.000 title 1
- 238000006731 degradation reaction Methods 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 238000000034 method Methods 0.000 title 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662425204P | 2016-11-22 | 2016-11-22 | |
PCT/US2017/063011 WO2018098275A1 (en) | 2016-11-22 | 2017-11-22 | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
Publications (3)
Publication Number | Publication Date |
---|---|
EP3544975A1 EP3544975A1 (en) | 2019-10-02 |
EP3544975A4 true EP3544975A4 (en) | 2020-07-01 |
EP3544975B1 EP3544975B1 (en) | 2022-01-05 |
Family
ID=62195645
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17873155.0A Active EP3544975B1 (en) | 2016-11-22 | 2017-11-22 | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and use |
Country Status (7)
Country | Link |
---|---|
US (1) | US10842878B2 (en) |
EP (1) | EP3544975B1 (en) |
JP (1) | JP7038712B2 (en) |
KR (1) | KR102566109B1 (en) |
AU (1) | AU2017363252B2 (en) |
CA (1) | CA3042297A1 (en) |
WO (1) | WO2018098275A1 (en) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11395820B2 (en) | 2016-03-16 | 2022-07-26 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Small molecules against cereblon to enhance effector t cell function |
CA3034326A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
JP2020525411A (en) | 2017-06-26 | 2020-08-27 | ベイジーン リミテッド | Immunotherapy for hepatocellular carcinoma |
US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
AU2019210748B2 (en) * | 2018-01-29 | 2021-08-05 | Dana-Farber Cancer Institute, Inc. | Degradation of Bruton's tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use |
CA3105506A1 (en) | 2018-07-11 | 2020-01-16 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Dimeric immuno-modulatory compounds against cereblon-based mechanisms |
WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
MX2021004191A (en) * | 2018-10-15 | 2021-05-27 | Nurix Therapeutics Inc | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway. |
WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
AU2020241903A1 (en) | 2019-03-21 | 2021-10-14 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
BR112021019722A2 (en) | 2019-04-09 | 2021-12-14 | Nurix Therapeutics Inc | 3-Substituted piperidine compounds for cbl-b inhibition, and use of cbl-b inhibitor in combination with cancer and/or oncolytic virus vaccine |
WO2020236654A1 (en) | 2019-05-17 | 2020-11-26 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof |
CN114364670A (en) | 2019-06-26 | 2022-04-15 | 纽力克斯治疗公司 | Substituted benzyl-triazoles for Cbl-b inhibition and further uses thereof |
CN114867727A (en) | 2019-07-17 | 2022-08-05 | 阿尔维纳斯运营股份有限公司 | TAU protein targeting compounds and related methods of use |
US20220281876A1 (en) * | 2019-07-26 | 2022-09-08 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
EP4055019A1 (en) * | 2019-11-08 | 2022-09-14 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
MX2022006672A (en) | 2019-12-04 | 2022-08-08 | Nurix Therapeutics Inc | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway. |
BR112022012385A2 (en) * | 2019-12-23 | 2022-08-30 | Shanghai Jemincare Pharmaceuticals Co Ltd | METHOD OF PREPARATION AND APPLICATION OF PROTEIN DEGRADING AGENT COMPOUND |
US20230211008A1 (en) * | 2020-03-31 | 2023-07-06 | Orum Therapeutics, Inc. | Conjugates |
WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
CA3186981A1 (en) | 2020-06-12 | 2021-12-16 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Phthalazinone compound, and preparation method therefor and medical use thereof |
CN113943293A (en) * | 2020-07-16 | 2022-01-18 | 百济神州(北京)生物科技有限公司 | Process for preparing bifunctional compounds as PROTAC BTK degraders |
WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
JP2024504932A (en) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス, インコーポレイテッド | isoindolinone compound |
IL305860A (en) | 2021-04-16 | 2023-11-01 | Arvinas Operations Inc | Modulators of bcl6 proteolysis and associated methods of use |
WO2023125908A1 (en) * | 2021-12-30 | 2023-07-06 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
CN114853735B (en) * | 2022-07-06 | 2022-10-21 | 北京鑫开元医药科技有限公司 | Compound for target ubiquitination degradation of TRK and preparation method, composition and application thereof |
US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
CN116283929B (en) * | 2023-01-10 | 2023-11-07 | 暨南大学 | Compounds inducing EGFR degradation and uses thereof |
Citations (4)
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WO2006099075A2 (en) * | 2005-03-10 | 2006-09-21 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
WO2009039397A2 (en) * | 2007-09-20 | 2009-03-26 | Cgi Pharmaceuticals, Inc. | Substituted amides, methods of making, use thereof for the treatment of diseases such as cancer |
WO2009137596A1 (en) * | 2008-05-06 | 2009-11-12 | Cgi Pharmaceuticals, Inc. | Substituted amides, method of making, and use as btk inhibitors |
US20160176916A1 (en) * | 2014-12-23 | 2016-06-23 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101523451B1 (en) * | 2008-07-02 | 2015-05-27 | 에프. 호프만-라 로슈 아게 | Novel phenylpyrazinones as kinase inhibitors |
JP2013104687A (en) * | 2011-11-10 | 2013-05-30 | Carna Biosciences Inc | Novel fluorescent probe and novel method for screening kinase inhibitor |
BR112014017095A2 (en) * | 2012-01-12 | 2017-06-13 | Yale University | compound, pharmaceutical composition, method for regulating protein activity of a target protein, method for treating a disease state or condition, library of a compound, method for degrading a target protein, and use of a compound |
RU2020139890A (en) * | 2014-04-14 | 2022-01-18 | Арвинас Оперэйшнз, Инк. | IMIDE MODULATORS OF PROTEOLYSIS AND METHODS FOR THEIR APPLICATION |
WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
CN108601764A (en) * | 2015-03-18 | 2018-09-28 | 阿尔维纳斯股份有限公司 | The Compounds and methods for of enhancing degradation for target protein |
GB201506871D0 (en) * | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
-
2017
- 2017-11-22 EP EP17873155.0A patent/EP3544975B1/en active Active
- 2017-11-22 CA CA3042297A patent/CA3042297A1/en active Pending
- 2017-11-22 US US16/343,974 patent/US10842878B2/en active Active
- 2017-11-22 WO PCT/US2017/063011 patent/WO2018098275A1/en unknown
- 2017-11-22 AU AU2017363252A patent/AU2017363252B2/en not_active Ceased
- 2017-11-22 KR KR1020197018105A patent/KR102566109B1/en active IP Right Grant
- 2017-11-22 JP JP2019527335A patent/JP7038712B2/en active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006099075A2 (en) * | 2005-03-10 | 2006-09-21 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
WO2009039397A2 (en) * | 2007-09-20 | 2009-03-26 | Cgi Pharmaceuticals, Inc. | Substituted amides, methods of making, use thereof for the treatment of diseases such as cancer |
WO2009137596A1 (en) * | 2008-05-06 | 2009-11-12 | Cgi Pharmaceuticals, Inc. | Substituted amides, method of making, and use as btk inhibitors |
US20160176916A1 (en) * | 2014-12-23 | 2016-06-23 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
Also Published As
Publication number | Publication date |
---|---|
AU2017363252A1 (en) | 2019-05-16 |
KR20190077595A (en) | 2019-07-03 |
AU2017363252B2 (en) | 2021-08-19 |
CA3042297A1 (en) | 2018-05-31 |
EP3544975B1 (en) | 2022-01-05 |
WO2018098275A1 (en) | 2018-05-31 |
JP7038712B2 (en) | 2022-03-18 |
KR102566109B1 (en) | 2023-08-10 |
JP2019535744A (en) | 2019-12-12 |
US20190262458A1 (en) | 2019-08-29 |
US10842878B2 (en) | 2020-11-24 |
EP3544975A1 (en) | 2019-10-02 |
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Ipc: C07D 401/14 20060101ALI20200528BHEP Ipc: C07D 417/12 20060101ALI20200528BHEP Ipc: A61K 31/454 20060101ALI20200528BHEP Ipc: A61K 31/497 20060101ALI20200528BHEP Ipc: C07D 417/14 20060101ALI20200528BHEP Ipc: A61P 35/00 20060101ALI20200528BHEP Ipc: C07D 403/12 20060101AFI20200528BHEP Ipc: A61K 31/427 20060101ALI20200528BHEP Ipc: C07D 401/04 20060101ALI20200528BHEP Ipc: A61K 47/54 20170101ALI20200528BHEP Ipc: A61K 47/55 20170101ALI20200528BHEP |
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